[go: up one dir, main page]

AR096927A1 - POWERFUL AND SELECTIVE INHIBITORS OF NaV1.7 - Google Patents

POWERFUL AND SELECTIVE INHIBITORS OF NaV1.7

Info

Publication number
AR096927A1
AR096927A1 ARP140100912A ARP140100912A AR096927A1 AR 096927 A1 AR096927 A1 AR 096927A1 AR P140100912 A ARP140100912 A AR P140100912A AR P140100912 A ARP140100912 A AR P140100912A AR 096927 A1 AR096927 A1 AR 096927A1
Authority
AR
Argentina
Prior art keywords
residue
amino acid
nal
secys
cys
Prior art date
Application number
ARP140100912A
Other languages
Spanish (es)
Inventor
Wanska Malgorzata
M Tegley Christopher
R Falsey James
M Doherty Elizabeth
P Miranda Leslie
Biswas Kaustav
C Long Jason
K Murray Justin
Ryan Holder Jerry
Sham Kelvin
Wu Bin
Original Assignee
Amgen Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Amgen Inc filed Critical Amgen Inc
Publication of AR096927A1 publication Critical patent/AR096927A1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/43504—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from invertebrates
    • C07K14/43513—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from invertebrates from arachnidae
    • C07K14/43518—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from invertebrates from arachnidae from spiders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/56—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/6811—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
    • A61K47/6817—Toxins
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/705—Receptors; Cell surface antigens; Cell surface determinants
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/44—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material not provided for elsewhere, e.g. haptens, metals, DNA, RNA, amino acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Toxicology (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Insects & Arthropods (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Zoology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Cell Biology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Se describe una composición de la materia, la cual comprende un polipéptido aislado, el cual es un inhibidor de NaV1.7 restringido periféricamente. En algunas realizaciones que se dan a conocer, el polipéptido aislado es un inhibidor de NaV1.7. Otras realizaciones son realizaciones conjugadas de la composición de la materia de la solicitud y composiciones farmacéuticas que contienen la composición de la materia de la solicitud. Se dan a conocer ácidos nucleicos aislados que codifican algunas realizaciones de polipéptidos y vectores de expresión de la solicitud, así como células huésped recombinantes que los contienen. También se da a conocer un método para tratar o prevenir el dolor. Reivindicación 1: Una composición de Ia materia, la cual comprende un polipéptido aislado que comprende la secuencia de aminoácidos de fórmula: Xaa¹Xaa²Xaa³Xaa⁴Xaa⁵Xaa⁶Xaa⁷Xaa⁸Xaa⁹Xaa¹⁰Xaa¹¹Asp¹²Xaa¹³Xaa¹⁴Xaa¹⁵Xaa¹⁶Xaa¹⁷Xaa¹⁸Xaa¹⁹Xaa²⁰Leu²¹Xaa²²Xaa²³Xaa²⁴Xaa²⁵Xaa²⁶Xaa²⁷Xaa²⁸Xaa²⁹Xaa³⁰Xaa³¹Xaa³²Xaa³³Xaa³⁴ // SEQ. ID Nº 590 o una sal farmacéuticamente aceptable del mismo, en donde: Xaa¹Xaa² está ausente; o Xaa¹ es cualquier residuo aminoacídico y Xaa² es cualquier residuo aminoacídico; o Xaa¹ está ausente y Xaa² es cualquier residuo aminoacídico; o Xaa¹ está ausente y Xaa² está ausente; Xaa³ es cualquier residuo aminoacídico; Xaa⁴ es Cys, si Xaa¹⁸ es Cys; o Xaa⁴ es SeCys, si Xaa¹⁸ es SeCys; Xaa⁵ es cualquier residuo aminoacídico hidrofílico neutro o básico; Xaa⁶ es cualquier residuo aminoacídico básico o hidrofílico neutro; Xaa⁷ es un residuo Trp, 5-bromoTrp, 6-bromoTrp, 5-cloroTrp, 6-cloroTrp, 1-Nal, 2-Nal, tioTrp, BhPhe, 2-BrhF, 2-ClhF, 2-FhF, 2-MehF, 2-MeOhF, 3-BrhF, 3-ClhF, 3-FhF, 3-MehF, 3-MeOhF, 4-BrhF, 4-ClhF, 4-FhF, 4-Me-F, 4-MehF, 4-MeOhF; Xaa⁸ es un residuo Met, Nle, Nva, Leu, Ile, Val, o Phe; Xaa⁹ es un residuo Trp, 5-bromoTrp, 6-bromoTrp, 5-cloroTrp, 6-cloroTrp, 1-Nal, 2-Nal, o tioTrp; Xaa¹⁰ es un residuo aminoacídico básico o hidrofílico neutro, o un residuo Ala; Xaa¹¹ es Cys si Xaa²³ es Cys; o Xaa¹¹ es SeCys si Xaa²³ es SeCys; Xaa¹³ es cualquier residuo aminoacídico; Xaa¹⁴ es un residuo básico o ácido o un residuo Ala; Xaa¹⁵ es un residuo Arg o Cit; Xaa¹⁶ es cualquier residuo aminoacídico; Xaa¹⁷ es Cys si Xaa²⁷ es Cys; o Xaa¹⁷ es SeCys si Xaa²⁷ es SeCys; Xaa¹⁸ es Cys o SeCys; Xaa¹⁹ es cualquier residuo aminoacídico; Xaa²⁰ es un residuo Gly, Asp o Ala; Xaa²² es un residuo aminoacídico ácido, básico o neutro hidrofílico, o un residuo Ala o Val; Xaa²³ es un residuo Cys o SeCys; Xaa²⁴ es un residuo aminoacídico básico o neutro hidrofílico o un residuo Ala; Xaa²⁵ es un residuo hidrofóbico alifático; Xaa²⁶ es un residuo Trp, 5-bromoTrp, 6-bromoTrp, 5-cloroTrp, 6-cloroTrp, 1-Nal, 2-Nal, tioTrp, 5-fenilTrp, 5-iPrTrp, 5-etilTrp, o 5-MeTrp; Xaa²⁷ es un residuo Cys o SeCys; Xaa²⁸ es un residuo aminoacídico básico o neutro hidrofílico; Xaa²⁹ es un residuo aminoacídico básico, o un residuo Tyr o Leu; Xaa³⁰ es un residuo Ile, Trp, Tyr, 5-bromoTrp, 6-bromoTrp, 5-cloroTrp, 6-cloroTrp, 1-Nal, 2-Nal, tioTrp, 1-Nal, o 2-Nal, si Xaa²² es un residuo aminoacídico ácido; o Xaa³⁰ es un residuo aminoacídico ácido o un residuo Pro, si Xaa²² es un residuo aminoacídico básico o neutro hidrofílico o un residuo Ala o Val; Xaa³¹ es un residuo Ile, Trp, Phe, Cha, Tyr, 5-bromoTrp, 6-bromoTrp, 5-cloroTrp, 6-cloroTrp, 1-Nal, 2-Nal, tioTrp, o 4-tBu-F; cada uno de Xaa³², Xaa³³, y Xaa³⁴ esté independientemente ausente o es en forma independiente un residuo aminoacídico ácido o hidrofóbico o un residuo Ser o Gly; y en donde: si Xaa⁴ y Xaa¹⁸ son ambos residuos Cys, existe un enlace disulfuro entre el residuo Xaa⁴ y el residuo Xaa¹⁸; o si Xaa⁴ y Xaa¹⁸ son ambos residuos SeCys, existe un enlace diseleniuro entre el residuo Xaa⁴ y el residuo Xaa¹⁸; si Xaa¹¹ y Xaa²³ son ambos residuos Cys, existe un enlace disulfuro entre el residuo Xaa¹¹ y el residuo Xaa²³; o si Xaa¹¹ y Xaa²³ son ambos residuos SeCys, existe un enlace diseleniuro entre el residuo Xaa¹¹ y el residuo Xaa²³; si Xaa¹⁷ y Xaa²⁷ son ambos residuos Cys, existe un enlace disulfuro entre el residuo Xaa¹⁷ y el residuo Xaa²⁷; o si Xaa¹⁷ y Xaa²⁷ son ambos residuos SeCys, existe un enlace diseleniuro entre el residuo Xaa¹⁷ y el residuo Xaa²⁷; el residuo amino terminal está opcionalmente acetilado, biotinilado o 4-pentinoilado, o PEGilado; y el residuo carboxi terminal está opcionalmente amidado.A composition of the matter is described, which comprises an isolated polypeptide, which is a peripherally restricted NaV1.7 inhibitor. In some embodiments that are disclosed, the isolated polypeptide is a NaV1.7 inhibitor. Other embodiments are conjugate embodiments of the composition of the subject matter of the application and pharmaceutical compositions containing the composition of the subject matter of the application. Isolated nucleic acids encoding some embodiments of polypeptides and expression vectors of the application, as well as recombinant host cells containing them are disclosed. A method for treating or preventing pain is also disclosed. Claim 1: A composition of the matter, comprising an isolated polypeptide comprising the amino acid sequence of formula: // Xaa¹Xaa²Xaa³Xaa⁴Xaa⁵Xaa⁶Xaa⁷Xaa⁸Xaa⁹Xaa¹⁰Xaa¹¹Asp¹²Xaa¹³Xaa¹⁴Xaa¹⁵Xaa¹⁶Xaa¹⁷Xaa¹⁸Xaa¹⁹Xaa²⁰Leu²¹Xaa²²Xaa²³Xaa²⁴Xaa²⁵Xaa²⁶Xaa²⁷Xaa²⁸Xaa²⁹Xaa³⁰Xaa³¹Xaa³²Xaa³³Xaa³⁴ SEQ. ID No. 590 or a pharmaceutically acceptable salt thereof, wherein: Xaa¹Xaa² is absent; or Xaa¹ is any amino acid residue and Xaa² is any amino acid residue; or Xaa¹ is absent and Xaa² is any amino acid residue; or Xaa¹ is absent and Xaa² is absent; Xaa³ is any amino acid residue; Xaa⁴ is Cys, if Xaa¹⁸ is Cys; or Xaa⁴ is SeCys, if Xaa¹⁸ is SeCys; Xaa⁵ is any neutral or basic hydrophilic amino acid residue; Xaa⁶ is any basic amino acid or hydrophilic neutral residue; Xaa⁷ is a residue Trp, 5-bromoTrp, 6-bromoTrp, 5-chloroTrp, 6-chloroTrp, 1-Nal, 2-Nal, thioTrp, BhPhe, 2-BrhF, 2-ClhF, 2-FhF, 2-MehF, 2-MeOhF, 3-BrhF, 3-ClhF, 3-FhF, 3-MehF, 3-MeOhF, 4-BrhF, 4-ClhF, 4-FhF, 4-Me-F, 4-MehF, 4-MeOhF; Xaa⁸ is a Met, Nle, Nva, Leu, Ile, Val, or Phe residue; Xaa⁹ is a Trp, 5-bromoTrp, 6-bromoTrp, 5-chloroTrp, 6-chloroTrp, 1-Nal, 2-Nal, or thioTrp residue; Xaa¹⁰ is a neutral or hydrophilic neutral amino acid residue, or an Ala residue; Xaa¹¹ is Cys if Xaa²³ is Cys; or Xaa¹¹ is SeCys if Xaa²³ is SeCys; Xaa¹³ is any amino acid residue; Xaa¹⁴ is a basic or acidic residue or an Ala residue; Xaa¹⁵ is an Arg or Cit residue; Xaa¹⁶ is any amino acid residue; Xaa¹⁷ is Cys if Xaa²⁷ is Cys; or Xaa¹⁷ is SeCys if Xaa²⁷ is SeCys; Xaa¹⁸ is Cys or SeCys; Xaa¹⁹ is any amino acid residue; Xaa²⁰ is a Gly, Asp or Ala residue; Xaa²² is an acidic, basic or neutral hydrophilic amino acid residue, or an Ala or Val residue; Xaa²³ is a Cys or SeCys residue; Xaa²⁴ is a hydrophilic basic or neutral amino acid residue or an Ala residue; Xaa²⁵ is an aliphatic hydrophobic residue; Xaa²⁶ is a Trp, 5-bromoTrp, 6-bromoTrp, 5-chloroTrp, 6-chloroTrp, 1-Nal, 2-Nal, thioTrp, 5-phenylTrp, 5-iPrTrp, 5-ethylTrp, or 5-MeTrp residue; Xaa²⁷ is a Cys or SeCys residue; Xaa²⁸ is a hydrophilic basic or neutral amino acid residue; Xaa²⁹ is a basic amino acid residue, or a Tyr or Leu residue; Xaa³⁰ is a residue Ile, Trp, Tyr, 5-bromoTrp, 6-bromoTrp, 5-chloroTrp, 6-chloroTrp, 1-Nal, 2-Nal, thioTrp, 1-Nal, or 2-Nal, if Xaa²² is a residue acidic amino acid; or Xaa³⁰ is an acidic amino acid residue or a Pro residue, if Xaa²² is a hydrophilic basic or neutral amino acid residue or an Ala or Val residue; Xaa³¹ is an Ile, Trp, Phe, Cha, Tyr, 5-bromoTrp, 6-bromoTrp, 5-chloroTrp, 6-chloroTrp, 1-Nal, 2-Nal, tioTrp, or 4-tBu-F residue; each of Xaa³², Xaa³³, and Xaa³⁴ is independently absent or is independently an acidic or hydrophobic amino acid residue or a Ser or Gly residue; and where: if Xaa⁴ and Xaa¹⁸ are both Cys residues, there is a disulfide bond between residue Xaa⁴ and residue Xaa¹⁸; or if Xaa⁴ and Xaa¹⁸ are both SeCys residues, there is a diselenide bond between the Xaa⁴ residue and the Xaa¹⁸ residue; if Xaa¹¹ and Xaa²³ are both Cys residues, there is a disulfide bond between residue Xaa¹¹ and residue Xaa²³; or if Xaa¹¹ and Xaa²³ are both SeCys residues, there is a diselenide bond between residue Xaa¹¹ and residue Xaa²³; if Xaa¹⁷ and Xaa²⁷ are both Cys residues, there is a disulfide bond between residue Xaa¹⁷ and residue Xaa²⁷; or if Xaa¹⁷ and Xaa²⁷ are both SeCys residues, there is a diselenide bond between residue Xaa¹⁷ and residue Xaa²⁷; the amino terminal residue is optionally acetylated, biotinylated or 4-pentinoylated, or PEGylated; and the carboxy terminal residue is optionally amidated.

ARP140100912A 2013-03-12 2014-03-12 POWERFUL AND SELECTIVE INHIBITORS OF NaV1.7 AR096927A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201361778331P 2013-03-12 2013-03-12

Publications (1)

Publication Number Publication Date
AR096927A1 true AR096927A1 (en) 2016-02-10

Family

ID=52343748

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP140100912A AR096927A1 (en) 2013-03-12 2014-03-12 POWERFUL AND SELECTIVE INHIBITORS OF NaV1.7

Country Status (2)

Country Link
US (1) US9636418B2 (en)
AR (1) AR096927A1 (en)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR096927A1 (en) 2013-03-12 2016-02-10 Amgen Inc POWERFUL AND SELECTIVE INHIBITORS OF NaV1.7
WO2014165277A2 (en) * 2013-03-12 2014-10-09 Amgen Inc. POTENT AND SELECTIVE INHIBITORS OF Nav1.7
CN110713530B (en) * 2018-07-12 2023-03-24 湖南师范大学 Application of sodium channel blocker mu-TRTX-Ca 1a as analgesic drug
US20220089663A1 (en) * 2019-01-18 2022-03-24 Memorial Sloan Kettering Cancer Center PROTEINS AND FLUOROPHORE-CONTAINING COMPOUNDS SELECTIVE FOR NaV1.7
CN111471092B (en) * 2020-04-11 2022-10-28 湖南师范大学 A spider polypeptide toxin with Nav1.9 specific activation and its application
US12347100B2 (en) 2020-11-19 2025-07-01 Mazor Robotics Ltd. Systems and methods for generating virtual images
CN113214362B (en) * 2021-05-18 2022-06-21 湖南百尔泰克化妆品有限公司 Polypeptide with inhibitory effect on sodium channel and application thereof
CN114805492B (en) * 2022-03-15 2025-07-22 上海元炘执药科技有限公司 Conotoxin KIIIA mutant for inhibiting voltage-gated sodium ion channel 1.4, and preparation method and application thereof
CN114805491B (en) * 2022-03-15 2025-10-03 青岛海洋生物医药研究院 A conotoxin KIIIA mutant and its preparation method and application
CN114917324B (en) * 2022-04-22 2025-05-30 江苏好上医生物医药有限公司 A pharmaceutical composition containing Huwentoxin-IV and its application
CN114957431B (en) * 2022-06-27 2023-06-20 四川丽妍工坊生物科技有限公司 Skin anti-wrinkle polypeptide Cj2a2, preparation method and application
CN120699106A (en) * 2024-03-26 2025-09-26 广州锡滔生物医药科技有限公司 A polypeptide and its application

Family Cites Families (56)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0640945A (en) 1992-07-23 1994-02-15 Kureha Chem Ind Co Ltd Fc fragment binding antitumor agent
US5432155A (en) 1993-06-29 1995-07-11 The Salk Institute For Biological Studies Conotoxins I
US5514774A (en) 1993-06-29 1996-05-07 University Of Utah Research Foundation Conotoxin peptides
US5756663A (en) 1996-01-03 1998-05-26 Zeneca Limited Antiarrhythmic peptide from venom of spider Grammostola spatulata
US5776896A (en) 1996-01-03 1998-07-07 Zeneca Limited Analgesic peptides from venom of grammostola spatulata and use thereof
AUPP589598A0 (en) 1998-09-14 1998-10-08 University Of Queensland, The Novel peptides
EP2112234A3 (en) 1999-11-26 2010-06-16 McGill University Loci for idiopathic generalized epilepsy, mutations thereof and method using same to assess, diagnose, prognose or treat epilepsy
CA2393616A1 (en) 2000-01-31 2001-08-02 Human Genome Sciences, Inc. Nucleic acids, proteins, and antibodies
US7125847B1 (en) 2000-04-07 2006-10-24 The Research Foundation Of State University Of New York At Buffalo Mechanically activated channel blocker
CN1133461C (en) 2000-04-11 2004-01-07 厦门北大之路生物工程有限公司 Application of Huwen bird spider toxin extract in preparation of analgesic medicine
EP1280895B1 (en) 2000-05-10 2005-08-03 Centre National De La Recherche Scientifique (Cnrs) Polypeptide inhibiting a proton-gated na+ channel
US7132505B1 (en) 2001-05-10 2006-11-07 Centre National De La Recherche Scientifique - Cnrs Polypeptide inhibiting a proton-gated Na+ channel, a nucleic acid coding for such polypeptide and a method of manufacturing an ASIC1a channel blocker
GB0021617D0 (en) 2000-09-02 2000-10-18 Imp College Innovations Ltd Diagnosis and treatment of cancer
CA2443968A1 (en) 2001-04-12 2002-10-24 Imperial College Innovations Limited Diagnosis and treatment of cancer: i
GB0120238D0 (en) 2001-08-20 2001-10-10 Univ College Of London Sodium channel regulators and modulators
AU2003219933A1 (en) 2002-02-25 2003-09-09 Vanderbilt University Expression system for human brain-specific voltage-gated sodium channel, type 1
US20040132101A1 (en) 2002-09-27 2004-07-08 Xencor Optimized Fc variants and methods for their generation
WO2003101972A1 (en) 2002-05-30 2003-12-11 The Scripps Research Institute Copper-catalysed ligation of azides and acetylenes
US7396816B2 (en) 2003-03-14 2008-07-08 Pharmadesign, Inc. Low-molecular weight peptides inhibiting ion channel activity
KR20060118398A (en) 2003-08-05 2006-11-23 버텍스 파마슈티칼스 인코포레이티드 Condensed Pyramidine Compounds as Voltage-gated Ion Channel Inhibitors
NZ579370A (en) 2003-08-08 2011-06-30 Vertex Pharma Heteroarylaminosulfonylphenyl derivatives for use as sodium or calcium channel blockers in the treatment of pain
US7615563B2 (en) 2003-08-08 2009-11-10 Gonzalez Iii Jesus E Compositions useful as inhibitors of voltage-gated sodium channels
US7060723B2 (en) 2003-08-29 2006-06-13 Allergan, Inc. Treating neurological disorders using selective antagonists of persistent sodium current
US7125908B2 (en) 2003-08-29 2006-10-24 Allergan, Inc. Treating pain using selective antagonists of persistent sodium current
AU2005207002B2 (en) 2004-01-21 2011-03-17 University Of Utah Research Foundation Mutant sodium channel Nav1.7 and methods related thereto
WO2005118614A1 (en) 2004-04-08 2005-12-15 Avigen, Inc. Methods and compositions for treating neuropathic pain
WO2006014493A2 (en) 2004-07-07 2006-02-09 The Research Foundation Of State University Of New York Stor Mechanically activated channel blocker
JO3000B1 (en) 2004-10-20 2016-09-05 Genentech Inc Antibody Formulations.
EP1809290A2 (en) 2004-11-03 2007-07-25 Vertex Pharmaceuticals Incorporated Pyrimidine derivatives as ion channel modulators and methods of use
WO2006101629A2 (en) 2005-02-17 2006-09-28 Vertex Pharmaceuticals Incorporated SODIUM CHANNEL PROTEIN TYPE III α-SUBUNIT SPLICE VARIANT
GB0517487D0 (en) 2005-08-26 2005-10-05 Isis Innovation Antibodies
US7972813B2 (en) 2005-09-30 2011-07-05 Vertex Pharmaceuticals Incorporated Tetrodotoxin-resistant sodium channel alpha subunit
US20120087969A1 (en) 2005-11-08 2012-04-12 Centre National De La Recherche Scientifique (C.N.R.S.) Mu-Conotoxin Peptides and Use Thereof as a Local Anesthetic
WO2007109324A2 (en) 2006-03-21 2007-09-27 Xenon Pharmaceuticals, Inc. Potent and selective nav 1.7 sodium channel blockers
JP4742345B2 (en) 2006-06-20 2011-08-10 独立行政法人産業技術総合研究所 Polypeptide derived from Gramostra spatula that blocks calcium channel and gene thereof
WO2007149542A2 (en) 2006-06-20 2007-12-27 Los Angeles Biomedical Research Institute At Harbor-Ucla Medical Center Antimicrobial kinocidin compositions and methods of use
CN100429229C (en) 2006-06-22 2008-10-29 湖南师范大学 Jingzhao toxin-V
WO2009033027A2 (en) 2007-09-05 2009-03-12 Medtronic, Inc. Suppression of scn9a gene expression and/or function for the treatment of pain
US8674071B2 (en) 2008-01-30 2014-03-18 Baylor College Of Medicine Peptides that target dorsal root ganglion neurons
CN101428138A (en) 2008-12-04 2009-05-13 深圳金蜘蛛生物科技有限公司 Uses of Chilobrachys jingzhao toxin extract-jingzhao toxin-V in preparing pain easing medicament
BRPI0924225A2 (en) 2009-02-02 2016-10-11 Chromocell Corp nav-expressing cell lines and methods of use
WO2010104114A1 (en) 2009-03-10 2010-09-16 独立行政法人産業技術総合研究所 Method for preparing polypeptide library
JPWO2010104115A1 (en) 2009-03-10 2012-09-13 独立行政法人産業技術総合研究所 Method for preparing a polypeptide that specifically recognizes a membrane protein
EP2432488A4 (en) 2009-03-20 2014-01-08 Amgen Inc Selective and potent peptide inhibitors of kv1.3
BR112012005860A2 (en) 2009-09-15 2017-01-31 Alomone Preclinical Ltd peptides isolated from spider venom, and uses thereof
WO2011051350A1 (en) 2009-10-27 2011-05-05 Ucb Pharma S.A. Function modifying nav 1.7 antibodies
GB0922435D0 (en) 2009-12-22 2010-02-03 Ucb Pharma Sa Method
GB0922434D0 (en) 2009-12-22 2010-02-03 Ucb Pharma Sa antibodies and fragments thereof
US8871996B2 (en) 2010-06-09 2014-10-28 Regeneron Pharmaceuticals, Inc. Mice expressing human voltage-gated sodium channels
WO2012004664A2 (en) 2010-07-07 2012-01-12 Purdue Pharma L.P. Analogs of sodium channel peptide toxin
SI2646470T1 (en) 2010-11-30 2017-05-31 F. Hoffmann-La Roche Ag Low affinity anti-transferrin receptor antibodies and their use to transfer therapeutic scfv across the blood brain barrier
HK1198173A1 (en) 2011-03-16 2015-03-13 Amgen Inc. Potent and selective inhibitors of nav1.3 and nav1.7
WO2013158800A1 (en) 2012-04-17 2013-10-24 University Of Utah Research Foundation Sodium channel sensitive conopeptides and analogs, including compositions and methods thereof
JP6771282B2 (en) 2012-05-18 2020-10-21 ヤンセン バイオテツク，インコーポレーテツド Fentoxin IV mutant and how to use it
US9644021B2 (en) 2013-01-11 2017-05-09 The California Institute For Biomedical Research Bovine fusion antibodies
AR096927A1 (en) 2013-03-12 2016-02-10 Amgen Inc POWERFUL AND SELECTIVE INHIBITORS OF NaV1.7

Also Published As

Publication number Publication date
US9636418B2 (en) 2017-05-02
US20150023988A1 (en) 2015-01-22

Similar Documents

Publication Publication Date Title
AR088413A1 (en) POWERFUL AND SELECTIVE INHIBITORS OF NaV1.3 AND NaV1.7
AR096927A1 (en) POWERFUL AND SELECTIVE INHIBITORS OF NaV1.7
CL2021002464A1 (en) Pharmaceutical composition, comprising the variant of human hyaluronidase ph20 and drug, for subcutaneous injection.
PE20081140A1 (en) THERAPEUTIC AGENTS BASED ON PEPTIDES DERIVED FROM TOXINS
AR110887A2 (en) CONSTANT MUTANT ANTIBODY REGION
AR110502A1 (en) ADENOVIRUS POLYUCLEOTIDES AND POLYPEPTIDES
AR064555A1 (en) WT1 PEPTIDE RESTRICTED TO HLA-A * 1101 AND PHARMACEUTICAL COMPOSITION THAT INCLUDES THE SAME
NZ606427A (en) Extended recombinant polypeptides and compositions comprising same
FI3642340T3 (en) MODIFIED L-ASPARAGINASE
RU2012101274A (en) Glucagon Compounds Active Against the GIP Receptor
PE20240015A1 (en) GDF15 FUSION PROTEINS AND USES OF THESE
HRP20190689T1 (en) Tear lipocalin muteins binding il-4 r alpha
CN106232616A (en) Amphiphilic synthetic antimicrobial peptide, its pharmaceutical composition and its use
CO2019013768A2 (en) Mic-1 compounds and their uses
NZ602634A (en) Vista regulatory t cell mediator protein, vista binding agents and use thereof
MX388822B (en) COMPOSITIONS COMPRISING PEPTIDE WKDEAGKPLVK.
HRP20150664T1 (en) ANTICANCEROGENIC FUSION PROTEIN
RU2017119773A (en) PEPTIDE ANTAGONISTS OF PEPTIDE HORMONES FROM THE CALCITONIN FAMILY (CGRP) AND THEIR APPLICATION
AR102324A1 (en) FHBP POLYPEPTIDES (FACTOR JOIN PROTEIN H) MODIFIED MENINGOCOCYCES
ATE517118T1 (en) BIS-MET HISTONES
RU2015103816A (en) CELLING PEPTIDES IN THE CELL, THE TARGET OF WHICH IS THE eIF4E
JP2017502003A5 (en)
US20180215804A1 (en) Reduction of inflammatory disease symptoms by short peptides that inhibit signaling through cd28
WO2012174397A3 (en) Anti-inflammatory pharmaceutical products
CU24746B1 (en) Human apyrases, solubilized and modified, useful for preventing and treating tissue damage

Legal Events

Date Code Title Description
FB Suspension of granting procedure